Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2003

Modified jatrophane diterpenes as modulators of multidrug resistance from Euphorbia dendroides L.

Résumé

The new diterpenoids terracinolides J-L (1-3), 13alpha-OH terracinolide F (8), abeodendroidin F (11) and epiabeodendroidin F (12) have been identified from Euphorbia dendroides L. The new compounds and six co-occurring known terracinolides were tested as inhibitors of the drug-efflux activity of P-glycoprotein from cancer cells. The results were used to extend the structure-activity relationships established for this class of compounds highlighting the relevance of substitution at positions 2, 3, 6, and 15 and disclosing a remarkable tolerance toward connectivity changes in the terpenoid core.The new diterpenoids terracinolides J-L (1-3), 13alpha-OH terracinolide F (8), abeodendroidin F (11) and epiabeodendroidin F (12) have been identified from Euphorbia dendroides L. The new compounds and six co-occurring known terracinolides were tested as inhibitors of the drug-efflux activity of P-glycoprotein from cancer cells. The results were used to extend the structure-activity relationships established for this class of compounds highlighting the relevance of substitution at positions 2, 3, 6, and 15 and disclosing a remarkable tolerance toward connectivity changes in the terpenoid core.
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Dates et versions

hal-00313605 , version 1 (27-08-2008)

Identifiants

  • HAL Id : hal-00313605 , version 1

Citer

G. Corea, E. Fattorusso, V. Lanzotti, O. Taglialatela-Scafati, G. Appendino, et al.. Modified jatrophane diterpenes as modulators of multidrug resistance from Euphorbia dendroides L.. Bioorganic and Medicinal Chemistry, 2003, 11, pp.5221-5227. ⟨hal-00313605⟩
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